BAYCOL
Clinical safety rating: caution
Comprehensive clinical and safety monograph for BAYCOL (BAYCOL).
Cerivastatin is a competitive inhibitor of HMG-CoA reductase, the rate-limiting enzyme in cholesterol biosynthesis, thereby reducing hepatic cholesterol production and increasing LDL receptor expression.
| Metabolism | Primarily metabolized by CYP3A4 and CYP2C8 to active metabolites; also undergoes glucuronidation. |
| Excretion | Renal: ~70% (mostly as unchanged drug); fecal: ~15% |
| Half-life | 2-4 hours (terminal elimination half-life); clinical context: supports twice-daily dosing |
| Protein binding | >99% (bound mainly to albumin and α1-acid glycoprotein) |
| Volume of Distribution | 0.3-0.5 L/kg (confined primarily to plasma and extracellular fluid) |
| Bioavailability | Oral: ~10% (extensive first-pass metabolism) |
| Onset of Action | Oral: 1-2 hours (serum cholesterol reduction begins) |
| Duration of Action | 12-24 hours (LDL-C reduction persists for 12-24 h with twice-daily dosing) |
Cervastatin 0.4 mg orally once daily in the evening, with or without food.
| Dosage form | TABLET |
| Renal impairment | Contraindicated in patients with severe renal impairment (CrCl < 30 mL/min); no specific dose adjustment for mild to moderate impairment (CrCl 30-80 mL/min). |
| Liver impairment | Contraindicated in patients with active liver disease or unexplained persistent elevations of serum transaminases; no Child-Pugh based adjustments available. |
| Pediatric use | Not approved for use in pediatric patients; safety and efficacy not established. |
| Geriatric use | No specific dose adjustment recommended; use caution due to potential for increased risk of adverse effects (e.g., myopathy). |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for BAYCOL (BAYCOL).
| Breastfeeding | Excretion in human milk unknown; not recommended due to potential for serious adverse effects in nursing infants. M/P ratio not established. |
| Teratogenic Risk | Pregnancy Category X. BAYCOL (cerivastatin) is contraindicated in pregnancy. Fetal risk includes skeletal malformations, CNS abnormalities, and reduced fetal growth due to inhibition of HMG-CoA reductase and reduced cholesterol synthesis. High risk in all trimesters. |
| Fetal Monitoring |
■ FDA Black Box Warning
Increased risk of rhabdomyolysis with renal failure, especially when used with gemfibrozil; contraindicated in combination with gemfibrozil.
| Serious Effects |
["Hypersensitivity to cerivastatin","Active liver disease or unexplained persistent transaminase elevations","Concomitant use with gemfibrozil","Pregnancy and lactation"]
| Precautions | ["Rhabdomyolysis and myopathy risk","Renal impairment","Hepatic effects (elevated transaminases)","Drug interactions with CYP3A4 inhibitors and gemfibrozil"] |
| Food/Dietary | Avoid grapefruit juice as it can increase cerivastatin blood levels and risk of side effects. Limit alcohol consumption due to potential liver effects. |
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| Not applicable as contraindicated in pregnancy. If inadvertent exposure occurs, monitor fetal growth and anatomy via ultrasound. |
| Fertility Effects | No human data; animal studies show reduced fertility and impaired spermatogenesis at high doses. Potential for negative impact on reproductive function. |
| Clinical Pearls |
| Baycol (cerivastatin) was withdrawn from the market in 2001 due to increased risk of rhabdomyolysis, especially when used with gemfibrozil. Monitor for unexplained muscle pain, tenderness, or weakness; measure CK levels if symptoms occur. Avoid coadministration with gemfibrozil; caution with other fibrates, niacin, and CYP3A4 inhibitors. |
| Patient Advice | Baycol has been withdrawn from the market and should not be used. · If you have been prescribed cerivastatin, contact your healthcare provider immediately for alternative cholesterol-lowering medication. · Report any unexplained muscle pain, tenderness, or weakness, especially if accompanied by fever or dark urine. · Do not take gemfibrozil or other fibrates with any statin without consulting your doctor. |